[Characteristics of T-593, a novel antiulcer agent, and each of its enantiomers on pharmacodynamics]
| Autor: | Hirotoshi Arai, Yukio Mori, Noriko Urata, Midori Mizuo, Norihisa Komae, Yasuko Doi |
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| Rok vydání: | 1998 |
| Předmět: |
Ulcer healing
Male Peptic Ulcer Pharmacology Guanidines Lethal Dose 50 Rats Sprague-Dawley Acetic acid chemistry.chemical_compound Structure-Activity Relationship Potency Animals Sulfones Rats Wistar Dose-Response Relationship Drug Ulcer recurrence Chemistry Chronic gastric ulcer Stereoisomerism Gastric mucosal blood flow Anti-Ulcer Agents Rats Histamine H2 Antagonists Gastric Mucosa Regional Blood Flow Pharmacodynamics Enantiomer |
| Zdroj: | Nihon yakurigaku zasshi. Folia pharmacologica Japonica. 112(2) |
| ISSN: | 0015-5691 |
| Popis: | T-593 consists of two optical isomers, (-)-S and (+)-R. Our previous report showed that T-593 has biphasic effects, that is a long-lasting antisecretory action and an improving effect on gastric mucosal blood flow (GMBF). In this study, we compared the sole potency of each isomer on these bi-phasic effects. On the anti-secretory action investigated by the pylorus-ligation method, the (-)-S-isomer showed strong inhibition, while the (+)-R-isomer showed no effect, whereas the GMBF improvement was provided by the (+)-R-isomer. These results show the bi-phasic effects of racemic T-593 are separately derived from each isomer. The (-)-S-isomer strongly inhibited acute gastric mucosal lesion formation, with a potency comparable to T-593 itself, while the (+)-R-isomer showed less effect. Chronic gastric ulcer induced by acetic acid was, however, not healed by the sole treatment of each optical isomer, while racemic T-593 showed a significant effect. This result shows not only anti-secretion but also GMBF improvement is necessary to heal the chronic ulcer. This interesting property of T-593 is expected to raise the quality of ulcer healing (QOUH) and also may prevent ulcer recurrence. |
| Databáze: | OpenAIRE |
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